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Reagents and reaction conditions: (i) NaH, THF, 0 °C to RT, 12 h; (ii) MgBr2·OEt, DIPEA, DCM, RT, 12 h; (iii) 3-chloroacetopheone, morpholine or 1-methyl-piperazine, Pd2 (dba)3, DavePhos, K3PO4, DME, Ar, 100 °C, 12 h; (iv) LiN(SiMe3)2, Ar, THF, −40 °C, 6 h; (v) (a) 2-methoxypropene, p-TSA, THF, RT, 1 h. (b) LiN(SiMe3)2, Ar, THF, −40 °C, 6 h, (c) HCl; vi) NH2NH2·H2O, ethanol, RT, 12 h.
